Olopatadine Hydrochloride

Modify Date: 2024-01-02 17:44:51

Olopatadine Hydrochloride Structure
Olopatadine Hydrochloride structure
Common Name Olopatadine Hydrochloride
CAS Number 140462-76-6 Molecular Weight 373.873
Density 1.221 g/cm3 Boiling Point 523ºC at 760mmHg
Molecular Formula C21H24ClNO3 Melting Point 242-245ºC
MSDS Chinese USA Flash Point 270.1ºC
Symbol GHS06 GHS09
GHS06, GHS09
Signal Word Danger

 Use of Olopatadine Hydrochloride


Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis.Target: Histamine ReceptorOlopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine significantly inhibited the ear swelling and the increased production of IL-4, IL-1beta, IL-6, GM-CSF and NGF in the lesioned ear [1]. Olopatadine was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials [2]. AL-4943A inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Passive anaphylaxis in guinea pig conjunctiva was attenuated by AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively) [3].

 Names

Name Olopatadine Hydrochloride
Synonym More Synonyms

 Olopatadine Hydrochloride Biological Activity

Description Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis.Target: Histamine ReceptorOlopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine significantly inhibited the ear swelling and the increased production of IL-4, IL-1beta, IL-6, GM-CSF and NGF in the lesioned ear [1]. Olopatadine was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials [2]. AL-4943A inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Passive anaphylaxis in guinea pig conjunctiva was attenuated by AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively) [3].
Related Catalog
References

[1]. Tamura, T., et al., Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice. Pharmacology, 2005. 75(1): p. 45-52.

[2]. Ohmori, K., et al., Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Jpn J Pharmacol, 2002. 88(4): p. 379-97.

[3]. Yanni, J.M., et al., The in vitro and in vivo ocular pharmacology of olopatadine (AL-4943A), an effective anti-allergic/antihistaminic agent. J Ocul Pharmacol Ther, 1996. 12(4): p. 389-400.

 Chemical & Physical Properties

Density 1.221 g/cm3
Boiling Point 523ºC at 760mmHg
Melting Point 242-245ºC
Molecular Formula C21H24ClNO3
Molecular Weight 373.873
Flash Point 270.1ºC
Exact Mass 373.144470
PSA 49.77000
LogP 4.39150
Vapour Pressure 9.65E-13mmHg at 25°C
Storage condition Refrigerator

 Safety Information

Symbol GHS06 GHS09
GHS06, GHS09
Signal Word Danger
Hazard Statements H301-H400
Precautionary Statements P273-P301 + P310
Hazard Codes T,N
Risk Phrases 25-50
Safety Phrases 45-61
RIDADR UN 2811 6.1 / PGIII
HS Code 2932999099

 Synthetic Route

 Customs

HS Code 2932999099
Summary 2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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 Synonyms

AL 4943A
MFCD00875716
Olopatadine hydrochloride
Dibenz[b,e]oxepin-2-acetic acid, 11-[3-(dimethylamino)propylidene]-6,11-dihydro-, (11Z)-, hydrochloride (1:1)
{(11Z)-11-[3-(Dimethylamino)propylidene]-6,11-dihydrodibenzo[b,e]oxepin-2-yl}acetic acid hydrochloride
{(11Z)-11-[3-(Dimethylamino)propyliden]-6,11-dihydrodibenzo[b,e]oxepin-2-yl}essigsäurehydrochlorid
{(11Z)-11-[3-(Dimethylamino)propylidene]-6,11-dihydrodibenzo[b,e]oxepin-2-yl}acetic acid hydrochloride (1:1)
dibenz[b,e]oxepin-2-acetic acid, 11-[3-(dimethylamino)propylidene]-6,11-dihydro-, (11Z)-, hydrochloride
acide {(11Z)-11-[3-(diméthylamino)propylidène]-6,11-dihydrodibenzo[b,e]oxépin-2-yl}acétique chlorhydrate
Olopatadine (hydrochloride)
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